The following information is provided to assist the reader in understanding technologies disclosed below and the environment in which such technologies may typically be used. The terms used herein are not intended to be limited to any particular narrow interpretation unless clearly stated otherwise in this document. References set forth herein may facilitate understanding of the technologies or the background thereof. The disclosure of all references cited herein are incorporated by reference.
Poor water solubility is one of the major hurdles for the advancement of drug candidates into clinical applications. Most drug companies focus on orally deliverable drugs. Not all drugs are orally bioavailable, however. Bioavailability may, for example, be defined as the fraction of an administered dose of unchanged drug that reaches, for example, the systemic circulation. Some compounds/drugs maybe degraded in the digest tract, some maybe too harmful for the epithelial lining, and in many cases, the duration of the free drug in blood once absorbed is very short. Any one or combination of these problems for a drug candidate may result in the elimination or cessation of drug development (as a general practice in the pharmaceutical industry).
Compound dispersion and/or solubilization are thus essential first steps for many pharmaceutical agents to be administered/absorbed by body, whether it is through an oral, a topical or a systemic route. Amphiphilic agents (which have a hydrophilic segment or head and a hydrophobic segment or tail) such as surfactants and various lipid-based formulations, such as micelles, emulsion, cream, liposome, solid-lipid nanoparticles are frequently used formulation systems for poorly soluble drugs. Lipidic based formulations, such as liposomes, emulsions and micelles, are attractive drug delivery systems for in vivo applications because of their excellent safety profiles. Water-soluble polymers, polymer-based hydrogels, and polymer-nanoparticles are also useful drug delivery systems for oral, topical and systemic use.
Various types of lipidic drug formulations are currently used in a clinical setting for the treatment of cancers and infectious diseases. Current approaches for determining lipidic formulations use trial and error process by selecting proper starting materials from existing off-shelf ingredients. Even for a more sophisticated work on synthetic molecules as a carrier, formulations are still empirical and not mechanistically based.